专利号:US-2023248849-A1 优先权日:2020-07-27 标 题:Contrast agents for detection of enzyme activities based on melanin synthesis 发明人:PAGEL MARK D 权利人:UNIV TEXAS 摘要:We disclose a composition, comprising a compound, comprising a melanin precursor that spontaneously synthesizes a melanin when in free form in vivo, and a peptide directly covalently bonded to or indirectly linked to the melanin precursor, wherein the direct covalent bond or indirect link of the peptide to the melanin precursor blocks spontaneous synthesis of the melanin in vivo in the absence of protease activity. We also disclose methods of tumor imaging, tumor detection, diagnosis, and treatment, including methods comprising administering, to a patient suffering from a tumor, the composition; and either surgically resecting the tumor or thermally ablating the tumor, wherein the surgical resection is guided at least in part by contrast imparted by, or the thermally ablating targets cells containing, the melanin, wherein the melanin is spontaneously synthesized in the tumor after administering the composition.
专利号:US-6123959-A 优先权日:1998-04-24 标题:Aqueous composition comprising active ingredients for the de-pigmentation of the skin 发明人:JONES KENNETH; PADMAPRIYA ABEYSINGHE; TEICHMUELLER ERNST E; BLUME GABRIELE 权利人:UNIVERA PHARM INC; ROVI GMBH 摘要:The present invention discloses aqueous compositions comprising liposomes of phospholipids, and at least one competitive inhibitor of an enzyme for the synthesis of melanin, in combination with at least one non-competitive inhibitor of an enzyme for the synthesis of melanin. The invention also includes the use of the compositions of this invention for the de-pigmentation of skin.
专利号:US-9512250-B2 优先权日:2012-02-23 标 题 :Manganese catalyzed photopolymerization of fluorinated monomers 发明人:ASANDEI ALEXANDRU D 权利人:UNIV CONNECTICUT 摘要:The disclosure discloses initiating systems for the radical polymerization of alkenes, and especially fluorine substituted alkenes. The polymerization is catalyzed by a metal carbonyl, preferably manganese carbonyl. The polymerization is initiated directly from alkyl halides at room temperature under visible white light. The polymers also allow the synthesis of block copolymers. The process comprises polymerizing at least one alkene monomer in the presence of a halide radical initiator, carbonyl catalyst and a solvent, under reaction conditions and for a time sufficient to polymerize the at least one alkene monomer to form a polymer. The present disclosure provides a method for living polymerization of alkene monomers which provides a high level of macromolecular control over the polymerization process and which leads to uniform and controllable polymeric products. This disclosure also provides a method for activating any halide (Cl, Br, I) chain ends of such polymers for the synthesis of block copolymerizations.
专利号:US-5801047-A 优先权日:1992-11-25 标题:Method for making stable extracellular tyrosinase and synthesis of polyphenolic polymers therefrom 发明人:DELLA-CIOPPA GUY RICHARD; GARGER JR STEPHEN JOHN; HOLTZ RICHARD BARRY; MCCULLOCH MICHAEL JAY; SVERLOW GENADIE GLEB 权利人:BIOSOURCE TECH INC 摘要:A process for the in vitro production of chemically modified polyphenolic polymer (PPP). First, stable, highly active extracellular tyrosinase is produced from genetically transformed microorganism such as Streptomyces antibioticus. The tyrosinase is then incubated with a reaction substrate such as 1-tyrosine, hydrolyzed protein, or an oligopeptide in combination with 1-tyrosine. The ratio of the oligopeptide/tyrosine combination as well as variation in the concentration of tyrosinase can be used to modify the color, the molecular size, and the spectral absorbance properties of the PPP produced. Alternatively, or additionally, oxidants such as hydrogen peroxide or hypochlorite can be used to modify the color of the PPP, regardless of the method used to produce the PPP, and the PPP can subsequently be fractionated using molecular weight cut-off ultrafiltration. Organic solvents can also be used in the method of making PPP to produce PPPs having variable but reproducible physical properties.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-2005080260-A1 优先权日:2003-04-22 标 题 :Preparation of prodrugs for selective drug delivery 发明人:MILLS RANDELL L; WU GUO-ZHANG 摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
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合成参考文献
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